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    • 8. 发明授权
    • 1H-4(5)-substituted imidazole derivatives, their preparation and their use as histamine H3 receptor ligands
    • 1H-4(5) - 取代咪唑衍生物,其制备及其作为组胺H3受体配体的用途
    • US06355665B1
    • 2002-03-12
    • US09463012
    • 2000-03-14
    • Matthew John TozerSarkis Barret KalindjianIan Duncan LinneyKatherine Isabel Mary SteelMichael John PetherTracey Cooke
    • Matthew John TozerSarkis Barret KalindjianIan Duncan LinneyKatherine Isabel Mary SteelMichael John PetherTracey Cooke
    • C07D23354
    • C07D233/64C07D417/04
    • A compound of the formula wherein R2 is an optionally substituted Cz to Cg alkylene or alkylene chain; R3 is C2 to C15 optionally substituted hydrocarbyl; X is a bond or —NR4—, wherein R4 is hydrogen or non-aromatic C1 to C5 optionally substituted hydrocarbyl, or aryl(C1 to C3)alkyl, or a pharmaceutically acceptable salt thereof. A method of modifing histamine activity in a patient comprising administering to said patient a pharmaceutical composition containing an effective amount of a compound of formula wherein R1 is selected from C1 to C6 alkyl, C1 to C6 alkoxy, C1 to C6 alkylthio, carboxy, carboxy(C1 to C6)alkyl, formyl, C1 to C6 alkylcarbonyl, C1 to C6 alkylcarbonylalkoxy, nitro, trihalomethyl, hydroxy, amino, C1 to C6 alkylcarbonylalkoxy, nitro, trihalomethyl, hydroxy, amino, C1 to C6 alkylamino, di(C1 to C6 alkyl)amino, aryl, C1 to C6 alkylaryl, halo, sulfamoyl and cyano; R2 is optionally substituted C2 to C20 hydrocarbylene, in which one or more hydrogen atoms may be replaced by halogen atoms and up to 6 carbon atoms may be replaced by oxygen or nitrogen atoms, R2 being in the form of an optionally substituted C2 to C8 alkylene or alkenylene chain; R3 is hydrogen or C1 to C15 optionally substituted hydrocarbyl; X is a bond or —NR4—; and a is from 0 to 2, or a pharmaceutically acceptable salt thereof.
    • 化学式R 2的化合物是任选取代的C 1至C 8亚烷基或亚烷基链; R3是C2至C15任选取代的烃基; X是键或-NR 4 - ,其中R 4是氢或非芳族C 1至C 5任选取代的烃基或芳基(C 1至C 3)烷基或其药学上可接受的盐。1,一种修饰患者组胺活性的方法, 向所述患者施用含有有效量的蛔虫素R1化合物的药物组合物选自C1至C6烷基,C1至C6烷氧基,C1至C6烷硫基,羧基,羧基(C1至C6)烷基,甲酰基,C1至C6 烷基羰基,C 1至C 6烷基羰基烷氧基,硝基,三卤代甲基,羟基,氨基,C 1至C 6烷基羰基烷氧基,硝基,三卤甲基,羟基,氨基,C 1至C 6烷基氨基,二(C 1至C 6烷基)氨基,芳基,C 1至C 6烷基芳基, ,氨磺酰基和氰基; R2是任选取代的C 2至C 20亚烃基,其中一个或多个氢原子可以被卤素原子取代,并且最多6个碳原子可被氧或氮原子取代,R 2为任选取代的C 2至C 8亚烷基 或亚烯基链; R 3是氢或C 1至C 15任选取代的烃基; X是键或-NR4-; 和a为0至2,或其药学上可接受的盐。